Reaktion #1807714

Reaktionsgleichung

HOBt

(2S)-1-(tert-Butoxycarbonyl)-2-[1-hydroxy-2-(4-methoxyphenoxy)ethyl]pyrrolidine

N-(tert-butoxycarbonyl)-L-proline

DCC

N-methylmorpholine

→

title compound

Ausbeute 69.8%

(2S)-1-[N-(tert-Butoxycarbonyl)-L-prolyl]-2-[1-hydroxy- 2-(4-methoxyphenoxy)ethyl]pyrrolidine

Ausbeute 69.8%

Lösungsmittel

hydrochloric acid 1,4-dioxane

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeThe residue obtained by concentration
2. 2
   Sonstigedrying of the reaction mixture
3. 3
   workup.DISSOLUTIONwas dissolved in DMF (15 ml)
4. 4
   Sonstigesubjected to the condensation reaction

Vorschrift

(2S)-1-(tert-Butoxycarbonyl)-2-[1-hydroxy-2-(4-methoxyphenoxy)ethyl]pyrrolidine (1.57 g) was dissolved in 4N hydrochloric acid/1,4-dioxane (23 ml), and the mixture was stirred at room temperature for 1 hour. The residue obtained by concentration and drying of the reaction mixture was dissolved in DMF (15 ml), and subjected to the condensation reaction using N-(tert-butoxycarbonyl)-L-proline (1.00 g), N-methylmorpholine (0.51 ml), HOBt (0.75 g) and DCC (0.96 g) in the same manner as in Example 46-C) to give 1.41 g of the title compound.

Quelle